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This study was designed to investigate the efficacy of the antidepressant drug bupropion in the treatment of posttraumatic stress disorder (PTSD). Seventeen male combat veterans with chronic PTSD were treated with bupropion in an open-label fashion for 6 weeks. Patients were evaluated with the Clinical Global Impressions Scale for Improvement (CGI-I) at follow-up and rated blindly at baseline and posttreatment with the Clinician Administered PTSD Scale (CAPS), the Hamilton Rating Scale for Depression (HAM-D), and the Hamilton Rating Scale for Anxiety. Three patients discontinued bupropion prematurely because of side effects. Of the remaining 14 patients, 10 were classified as treatment responders by the CGI-I. HAM-D scores decreased significantly from baseline to follow-up. The improvement seen in hyperarousal symptoms was significant but was less significant than the change in depressive symptoms. There was no significant change in Intrusion, Avoidance, or total CAPS scores. It was concluded that bupropion was well tolerated. Patients who had experienced sexual dysfunction with selective serotonin reuptake inhibitors reported no complaints during bupropion treatment. Bupropion decreased depressive symptoms and most patients reported global improvement, although PTSD symptoms remained mostly unchanged. Controlled trials should further clarify the role of bupropion in the treatment of PTSD.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9790155&dopt=Abstract Bupropion Wellbutrin

GlaxoWellcome.com

BACKGROUND: The nicotine transdermal patch (NTP) has been shown previously to be a cost-effective smoking cessation intervention. This is the first economic analysis comparing the NTP with the only non-nicotine-containing pharmacological intervention, bupropion HCl. METHODS: Decision-tree analysis, based on a previously published cost-benefit smoking-cessation model, was used to determine the optimal treatment from the standpoint of costs versus benefits, from the employer's perspective. Base-case probabilities of successful quitting in our model came from clinical trial point-prevalence data at the end of a 1-year follow-up study (N = 893) comparing placebo, bupropion, NTP, and bupropion/NTP in combination, administered along with minimal counseling. Sensitivity analyses were performed to determine the effects of variations in base-case assumptions regarding the monetary benefits that would accrue if an intervention were successful, probabilities of quitting, drug costs, cost of lost work time for a health care provider visit, and cost of the visit itself. RESULTS: The analysis showed that bupropion is more cost-beneficial than either NTP or bupropion/NTP, with a net benefit in the first post-quit year of up to $338 per employee who attempts to quit compared with $26 for NTP, $178 for the two in combination, and $258 for placebo. These results were robust to most plausible variations in the assumptions used in the model. One exception was the monetary benefit of successful intervention (assumed in the base-case to be $1,654). If this benefit were actually less than $1, 112, placebo (i.e., minimal counseling with no pharmacological intervention) would be more cost-beneficial than any of the active treatmen




Psychopharmacology (Berl). 1992;106(2):248-52.
Effects of bupropion on core body temperature of mice.

Zarrindast MR, Abolfathi-Araghi F.

Department of Pharmacology, Medical Faculty, University of Tehran, Iran.

The effects of bupropion on core body temperature of intact or reserpinized mice were studied. Intraperitoneal (IP) administration of bupropion to mice induced a dose-dependent hypothermia. The response of bupropion was decreased by the D-2 antagonist sulpiride or pimozide, but not by the D-1 antagonist SCH 23390, antimuscarinic drug atropine, alpha-adrenergic blocker phenoxybenzimine, beta-adrenergic antagonist propranolol or antiserotonergic methergoline. Reserpine induced hypothermia, which was reversed by bupropion administration. The reversal response of bupropion was reduced by propranolol, but not sulpiride, SCH 23390, phenoxybenzamine, atropine or methergoline. It is concluded that bupropion-induced hypothermia may be mediated through D-2 receptor activation, while the reversal of reserpine-induced hypothermia by bupropion may be exerted through beta-adrenergic stimulation.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1347953&dopt=Abstract Bupropion Wellbutrin




Psychopharmacology (Berl). 1985;85(2):173-7.
Characterization of the bupropion cue in the rat: lack of evidence for a dopaminergic mechanism.

Blitzer RD, Becker RE.

Using a two-lever operant task rats were trained to discriminate 40 mg/kg IP of bupropion from saline. Despite bupropion's established dopaminergic activity in vitro and in vivo, it was found that the bupropion cue was neither mimicked by the dopaminergic drugs L-DOPA and bromocriptine nor blocked by a variety of neuroleptics (haloperidol, thioridazine, and thiothixene). In addition, bupropion was active in attenuating the behavior-suppressing effects of haloperidol, unlike amphetamine and the atypical antidepressants, nomifensine and viloxazine. The bupropion cue was not mimicked or disrupted by adrenergic or serotonergic drugs, but it did generalize to some stimulants (amphetamine, cocaine and caffeine) as well as to nomifensine and viloxazine. The generalizations were blocked by neuroleptics. These data indicate that bupropion's cue properties may not be based on its ability to modulate dopaminergic receptor activity. The possible involvement of phenylethylamine in the bupropion cue is also discussed.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2861618&dopt=Abstract Bupropion Wellbutrin




Drug Metab Dispos. 1986 Nov-Dec;14(6):692-7.
Pharmacokinetics of bupropion and metabolites in plasma and brain of rats, mice, and guinea pigs.

Suckow RF, Smith TM, Perumal AS, Cooper TB.

Recent reports indicate that bupropion, a novel non-tricyclic antidepressant, is metabolized differently in certain species of animals. To further define the disposition of bupropion, a study was done involving three species, the rat, mouse, and guinea pig, as animal models to evaluate bupropion metabolism. The pharmacokinetic profiles of bupropion and its major basic metabolites, BW 306U and BW A494U, were determined following the ip administration of 40 mg/kg bupropion to these animals. Pharmacokinetic profiles of the parent drug and metabolites from plasma and brain samples were obtained using a liquid chromatographic procedure. Further investigation of the reduced bupropion metabolite BW A494U was carried out by the ip administration of this metabolite to these animals and assaying the plasma and brain samples 90 min after dosing. Analysis of the pharmacokinetic data revealed that the rat quickly metabolized bupropion, but no basic metabolites accumulated. The mouse metabolized bupropion predominantly to BW 306U, whereas the guinea pig converted bupropion to reduced bupropion (BW A494U) as well as BW 306U. Brain/plasma ratios of bupropion among these animals did not vary significantly. However, both metabolites showed dramatic differences in their brain/plasma ratios among these species. When reduced bupropion (BW A494U) was injected, almost 3% of the plasma concentration of BW A494U was determined to be bupropion in the rat. Lesser amounts were converted in the mouse and guinea pig. Therefore, we have demonstrated that distinct differences exist in the metabolism of bupropion in various species of animals. The guinea pig, when compared to the rat or mouse, appears to constitute a model that most closely resembles that of human bupropion metabolism.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2877828&dopt=Abstract Bupropion Wellbutrin